An efficient synthesis of (R)- and (S)-baclofen via desymmetrization

A short and highly enantioselective synthesis of both enantiomers of GABA agonist baclofen in four steps with total yields of 32.8% [for(S)-isomer] and 35.1% [for (R)-isomer] is reported. The key step involved desymmetrization of cyclic anhydride with modified cinchona alkaloids. (C) 2009 Elsevier Ltd. All rights reserved.